Title: Assistant professor of medicinal chemistry
College/Institute: College of Pharmacy
Research interests: Organic compound synthesis, drug discovery, medicinal chemistry, antibacterial agents
Curriculum vitae: PDF
Hobbies: Power lifting, bench press enthusiast
Robert Huigens joined the College of Pharmacy and the EPI in 2013 where he pursues his passion for examining phenazine antibiotics and synthesizing novel compounds from natural products to discover therapeutic applications. His work as a synthetic chemist occurs at the interface of chemistry, medicine, and microbiology. “Our lab synthesizes compounds that have interesting antimicrobial or antibacterial activities,” Huigens says. “We are also interested in natural products, these are naturally occurring molecules found in nature. We are inspired by the microbial warfare strategies that bacteria and fungi use to compete for certain niches in the environment.”
His lab addresses the limitation of modern antibiotics in treating biofilm infections, and his goal is to develop small molecules that specifically target bacterial biofilms. Patients with certain diseases, such as drug-resistant tuberculosis are at high risk of developing biofilm infections, as are disease-free patients who have received a surgically implanted device. “There are biofilms everywhere, you can’t get away from them,” Huigens says. “We need to figure out how to control them.”
Whereas conventional antibiotics effectively kill bacteria in their planktonic (free-floating) state they are inefficient at destroying bacteria that have developed into a biofilm and adhered to surface. This is because conventional antibiotics target planktonic bacteria, but when these same bacteria form a biofilm they develop extracellular matrices that can tolerate antibiotics at hundreds of times the concentration needed to kill planktonic bacteria. “We have to find compounds that operate through new modes of action,” Huigens says.
In 2015, he had a major breakthrough when his lab discovered a halogenated phenazine compound capable of “potently killing” bacterial biofilms and methicillin-resistant Staphylococcus aureus (MRSA). It also demonstrated antibacterial activity against Mycobacterium tuberculosis, the pathogen that causes tuberculosis. Further research revealed the novel compound starves bacteria of iron uptake causing rapid cellular death. This is surprising considering that bacteria which have formed a biofilm are considered dormant. His lab is working to translate these findings into therapeutic applications.
In a separate project, Huigens’ lab uses a method called ring distortion to create novel compounds synthesized from natural products which are then screened for biological activity that may have antimicrobial or anticancer properties. By using high-throughput screening to examine small molecules with structural complexity – such as fused rings – his lab exploits an area that commercial pharmaceutical laboratories that typically overlook. “We take the original compound and change it dramatically by breaking carbon-nitrogen bonds,” Huigens explains. “This project makes compounds that are very different from the compounds currently being screened for drug discovery efforts. We are addressing the lack of stereochemical complexity in screening libraries.” The search has yielded promising new substances that will be announced after publication in 2019.
Dr. Huigens’ formal chemistry education took place at North Carolina State University where he credits professor Christian Melander with inspiring him on his current research path. He also flourished under an undergraduate professor, Terrence Nile, at the University of North Carolina-Greensboro “who taught chemistry like poetry” and influenced Huigens to change majors from a pre-medical track to chemistry. After completing an American Cancer Society postdoctoral fellowship at the University of Illinois at Urbana-Champaign with professor Paul Hergenrother, UF attracted Huigens. He says he is grateful for the opportunity to work in an interdisciplinary setting with a group like the EPI, and to be supported in pursuing chemistry at the interface of medicine and microbiology.
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